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Molecules. 2021 Nov 23;26(23). doi: 10.3390/molecules26237066.

Taurochenodeoxycholic Acid Increases cAMP Content via Specially Interacting with Bile Acid Receptor TGR5.

Molecules (Basel, Switzerland)

Youchao Qi, Linkai Shi, Guozhen Duan, Yonggui Ma, Peifeng Li

Affiliations

  1. Department of Basic Veterinary Medicine, College of Veterinary Medicine, Inner Mongolia Agricultural University, Hohhot 010010, China.
  2. Key Laboratory of Clinical Diagnosis and Treatment Techniques for Animal Disease, Ministry of Agriculture, Hohhot 010010, China.
  3. Department of Veterinary Medicine, College of Agriculture and Animal Husbandry, Qinghai University, Xining 810016, China.
  4. Agricultural and Pastoral Bureau of Togtoh County, Togtoh 010200, China.
  5. Academy of Agriculture and Forestry Sciences, Qinghai University, Xining 810016, China.
  6. Key Laboratory of Medicinal Animal and Plant Resources of Qinghai Tibetan Plateau, Qinghai Normal University, Xining 810008, China.
  7. Academy of Plateau Science and Sustainability, Qinghai Normal University, Xining 810008, China.

PMID: 34885648 PMCID: PMC8659238 DOI: 10.3390/molecules26237066

Abstract

Taurochenodeoxycholic acid (TCDCA) is one of the main components of bile acids (BAs). TCDCA has been reported as a signaling molecule, exerting anti-inflammatory and immunomodulatory functions. However, it is not well known whether those effects are mediated by TGR5. This study aimed to elucidate the interaction between TCDCA and TGR5. To achieve this aim, first, the TGR5 eukaryotic vector was constructed. The expression level of TGR5 in 293T cells was determined by immunofluorescence, real-time quantitative PCR (RT-PCR, qPCR), and Western blot. The luciferase assay, fluorescence microscopy, and enzyme-linked immunosorbent assay (ELISA) were recruited to check the interaction of TCDCA with TGR5. TCDCA treatment in 293T cells resulted in TGR5 internalization coupled with a significant increase in cAMP luciferase expression. Our results demonstrated that TCDCA was able to bind to the TGR5 receptor and activate it. These results provide an excellent potential therapeutic target for TCDCA research. Moreover, these findings also provide theoretical evidence for further TCDCA research.

Keywords: 239T cells; TGR5; cyclic adenosine monophosphate; interaction; taurochenodeoxycholic acid

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